2. Metabolic Enzyme/Protease Vitamin D Related/Nuclear Receptor Cell Cycle/DNA Damage Autophagy
  3. Phosphodiesterase (PDE) PPAR Autophagy
  4. Icariin

Icariin is a flavonol glycoside. Icariin inhibits PDE5 and PDE4 activities with IC50s of 432 nM and 73.50 μM, respectively. Icariin also is a PPARα activator.

For research use only. We do not sell to patients.

CAS No. : 489-32-7

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Customer Review

Based on 27 publication(s) in Google Scholar

Other Forms of Icariin:

Icariin Related Antibodies

Top Publications Citing Use of Products
Cell Imaging/Staining
WB
Cell Proliferation/Viability Assay

    Icariin purchased from MedChemExpress. Usage Cited in: Front Pharmacol. 2020 Mar 19;11:256.  [Abstract]

    As demonstrated by Masson staining, collagen deposition was reduced in the myocardium of Icariin (30 mg/kg)-treated db/db mice.

    Icariin purchased from MedChemExpress. Usage Cited in: Front Pharmacol. 2020 Mar 19;11:256.  [Abstract]

    The DHE staining indicated that Icariin (30 mg/kg) treatment alleviated the production of ROS in the myocardial tissue of db/db mice.

    Icariin purchased from MedChemExpress. Usage Cited in: Front Pharmacol. 2020 Mar 19;11:256.  [Abstract]

    TUNEL staining revealed that Icariin (30 mg/kg) treatment rescued the apoptotic rate of cardiomyocytes.

    Icariin purchased from MedChemExpress. Usage Cited in: Front Pharmacol. 2020 Mar 19;11:256.  [Abstract]

    The mitochondrial dynamics-related protein, Mfn2, mitochondrial biogenesis regulation protein, PGC‐1α, and mitochondrial gene, cytochrome-b (Cyt-b), were upregulated in the Icariin-treated (30 mg/kg) db/db mice.

    Icariin purchased from MedChemExpress. Usage Cited in: Front Pharmacol. 2020 Mar 19;11:256.  [Abstract]

    The number of HG-treated cardiomyocytes was significantly higher following incubation with Icariin for 12 h, 24 h, or 48 h at concentrations of 7.5, 15, or 30 µM.

    View All Phosphodiesterase (PDE) Isoform Specific Products:

    View All Isoforms
    PDE1 PDE2 PDE3 PDE4 PDE5 PDE6 PDE7 PDE9 PDE10 PDE11 PDE12 PDE8 Autotaxin

    View All PPAR Isoform Specific Products:

    View All Isoforms
    PPARα PPARβ/δ PPARγ PPAR PPARδ

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Icariin is a flavonol glycoside. Icariin inhibits PDE5 and PDE4 activities with IC50s of 432 nM and 73.50 μM, respectively. Icariin also is a PPARα activator.

    IC50 & Target[1][2]

    PDE5

    432 nM (IC50)

    PDE4

    73.5 μM (IC50)

    PPARα

     

    Autophagy

     

    Cellular Effect
    Cell Line Type Value Description References
    COS-7 IC50
    5.9 μM
    Compound: 1
    Inhibition of human recombinant PDE5A1 expressed in COS7 cells
    Inhibition of human recombinant PDE5A1 expressed in COS7 cells
    		[PMID: 18778098]
    NCI/ADR-RES IC50
    > 100 μM
    Compound: 1, icariin
    Cytotoxicity against human MCF7/ADR cells after 72 hrs by MTT assay
    Cytotoxicity against human MCF7/ADR cells after 72 hrs by MTT assay
    		[PMID: 19523827]
    TM3 CC50
    > 200 μM
    Compound: Icariin
    Cytotoxicity against mouse TM3 cells assessed as reduction in cell viability measured after 24 hrs by sulforhodamine B assay
    Cytotoxicity against mouse TM3 cells assessed as reduction in cell viability measured after 24 hrs by sulforhodamine B assay
    		[PMID: 31091478]
    In Vitro

    Icariin is a cGMP-specific PDE5 inhibitor. The inhibitory effects of Icariin on PDE5 and PDE4 activities are investigated by the two-step radioisotope procedure with 3H-cGMP/ 3H-cAMP. The potency of selectivity of Icariin on PDE5 (PDE4/PDE5 of IC50) is 167.67 times[1]. Cell viability is measured in the present study to evaluate whether Icariin protect endothelial HUVECs from injuries induced by oxidized low-density lipoprotein (ox-LDL). The exposure of the cells to ox-LDL for 24 h significantly decreases the cell viability compared with control group (P<0.05). However, Icariin can inhibit cell injury induced by ox-LDL in a concentration-dependent manner, and has significant difference (P<0.05) compared with ox-LDL-simulated group[3].
    Icariin protects BMSCs against OGD-induced apoptosis by inhibiting ERs-mediated (ER Stress) autophagy via MAPK signaling pathway[5].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Icariin Related Antibodies
    In Vivo

    Icariin is a PPARα activator, induces Cyp4a10 and Cyp4a14, and regulates the mRNA levels of lipid metabolism enzymes and proteins, including fatty acid binding protein, fatty acid oxidation in mitochondria and in peroxisome. Icariin is effective in the treatment of hyperlipidemia. To understand the effect of Icariin on lipid metabolism, effects of Icariin on PPARα and its target genes are investigated. Mice are treated orally with Icariin at doses of 0, 100, 200, and 400 mg/kg, or Clofibrate (500 mg/kg) for five days. Liver total RNA is isolated and the expressions of PPARα and lipid metabolism genes are examined. PPARα and its marker genes Cyp4a10 and Cyp4a14 are induced 2-4 fold by Icariin, and 4-8 fold by Clofibrate. The fatty acid (FA) binding and co-activator proteins Fabp1, Fabp4 and Acsl1 are increased 2-fold. The mRNAs of mitochondrial FA β-oxidation enzymes (Cpt1a, Acat1, Acad1 and Hmgcs2) are increased 2-3 fold. The mRNAs of proximal β-oxidation enzymes (Acox1, Ech1, and Ehhadh) are also increased by Icariin and Clofibrate. The expression of mRNAs for sterol regulatory element-binding factor-1 (Srebf1) and FA synthetase (Fasn) are unaltered by Icariin. The lipid lysis genes Lipe and Pnpla2 are increased by Icariin and Clofibrate[2]. Adult rats are treated orally with Icariin at doses of 0 (control), 50, 100, or 200 mg/kg body weight for 35 consecutive days. The results show that Icariin has virtually no effect on the body weight or organ coefficients of the testes or epididymides. However, 100 mg/kg Icariin significantly increases epididymal sperm counts. In addition, 50 and 100 mg/kg Icariin significantly increase testosterone levels. Furthermore, 100 mg/kg Icariin treatment also affects follicle stimulating hormone receptor (FSHR) and claudin-11 mRNA expression in Sertoli cells. Superoxide dismutase (SOD) activity and malondialdehyde (MDA) levels are measured in the testes; 50 and 100 mg/kg Icariin treatment improve antioxidative capacity, while 200 mg/kg Icariin treatment upregulates oxidative stress[4].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
    Clinical Trial
    Molecular Weight

    676.66

    Formula

    C33H40O15
    CAS No.
    Appearance

    Solid

    Color

    Light yellow to yellow

    SMILES

    O[C@H]1[C@H](O)[C@@H](CO)O[C@@H](OC2=C(C/C=C(C)/C)C(OC(C3=CC=C(OC)C=C3)=C(O[C@@H]4O[C@@H](C)[C@H](O)[C@@H](O)[C@H]4O)C5=O)=C5C(O)=C2)[C@@H]1O
    Structure Classification
    Initial Source
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    DMSO : 125 mg/mL (184.73 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.4778 mL 7.3892 mL 14.7785 mL
    5 mM 0.2956 mL 1.4778 mL 2.9557 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

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    Volume (start)

    V1

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    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    90% Corn Oil

      Solubility: ≥ 2.5 mg/mL (3.69 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

    • Protocol 2

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.08 mg/mL (3.07 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  50% PEG300    50% Saline

      Solubility: 10 mg/mL (14.78 mM); Suspended solution; Need ultrasonic

    • Protocol 2

      Add each solvent one by one:  0.5% CMC/saline water

      Solubility: 10 mg/mL (14.78 mM); Suspended solution; Need ultrasonic

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 99.06%

    SDS (393 KB)

    COA (259 KB) LCMS (267 KB)

    Handling Instructions (2659 KB)
    References
    Cell Assay
    [3]

    Human umbilical vein endothelial cells (HUVECs) in the logarithmic growth phase are seeded into 96-well plates at a density of 1×104 cells per well, then incubated for 24 hours at 37°C, 5% CO2. After pretreatment with indicated concentration of Icariin (0, 10, 20, 40 μM) for 24 hours, the cells are incubated with or without ox-LDL (100 μg/mL) for next 24 hours. After suction of the liquid in the wells, MTT solution is added to yield a final concentration of 0.5 mg/mL, and incubation is continued for 4 h at 37°C, 5% CO2. MTT solution is removed gently and 150 μL of DMSO is added to each well for 15 min incubation. The absorbance of each sample is measrured on a microplate reader at 490 nm as cell viability[3].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [2][4]

    Mice[2]
    Adult 8-week old male C57BL/6 mice are acclimated for 1-week in a temperature- and humidity-controlled facility with a standard 12-h light schedule. Mice have free access to SPF-grade rodent chow and purified drinking water. Mice are treated with Icariin (100, 200, and 400 mg/kg) for 5 days. Clofibrate (CLO, 500 mg/kg, po for 5 days) is used as a positive control, for negative controls, mice are given 2% CMC (10 mL/kg). 24 h after the last dose, livers are collected for analysis.
    Rats[4]
    Forty adult male SD rats weighing 200-290 g (12-16 weeks old) are randomly assigned to groups (n=10 per group) according to their body weight. The rats receive daily intragastric administration of Icariin at 0 (control), 50, 100, or 200 mg/kg per day for 35 consecutive days. The animals are weighed weekly, and the treatments are adjusted accordingly. At the end of the Icariin treatment period, all rats are sacrificed; blood samples are subsequently collected for further analyses of testosterone levels.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.4778 mL 7.3892 mL 14.7785 mL 36.9462 mL
    5 mM 0.2956 mL 1.4778 mL 2.9557 mL 7.3892 mL
    10 mM 0.1478 mL 0.7389 mL 1.4778 mL 3.6946 mL
    15 mM 0.0985 mL 0.4926 mL 0.9852 mL 2.4631 mL
    20 mM 0.0739 mL 0.3695 mL 0.7389 mL 1.8473 mL
    25 mM 0.0591 mL 0.2956 mL 0.5911 mL 1.4778 mL
    30 mM 0.0493 mL 0.2463 mL 0.4926 mL 1.2315 mL
    40 mM 0.0369 mL 0.1847 mL 0.3695 mL 0.9237 mL
    50 mM 0.0296 mL 0.1478 mL 0.2956 mL 0.7389 mL
    60 mM 0.0246 mL 0.1232 mL 0.2463 mL 0.6158 mL
    80 mM 0.0185 mL 0.0924 mL 0.1847 mL 0.4618 mL
    100 mM 0.0148 mL 0.0739 mL 0.1478 mL 0.3695 mL
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    Icariin Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    Icariin489-32-7IearilinePhosphodiesterase (PDE)PPARAutophagyPeroxisome proliferator-activated receptorsInhibitorinhibitorinhibit

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